Found 6 hits in this display Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
ADAMTS5
(Rattus norvegicus (Rat)) | BDBM429684
(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)Show SMILES Clc1cc(Cl)cc(c1)C1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1 Show InChI InChI=1S/C20H23Cl2N3O3/c21-15-9-13(10-16(22)11-15)12-4-7-25(8-5-12)17(26)3-6-20(14-1-2-14)18(27)23-19(28)24-20/h9-12,14H,1-8H2,(H2,23,24,27,28) | PDB
UniProtKB/TrEMBL
GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 75 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by rnADAMTS-5 (1-564-6H).For the d... |
US Patent US10550100 (2020)
BindingDB Entry DOI: 10.7270/Q2D2211N |
More data for this Ligand-Target Pair | |
A disintegrin and metalloproteinase with thrombospondin motifs 5
(Homo sapiens (Human)) | BDBM429684
(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)Show SMILES Clc1cc(Cl)cc(c1)C1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1 Show InChI InChI=1S/C20H23Cl2N3O3/c21-15-9-13(10-16(22)11-15)12-4-7-25(8-5-12)17(26)3-6-20(14-1-2-14)18(27)23-19(28)24-20/h9-12,14H,1-8H2,(H2,23,24,27,28) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 75 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by human ADAMTS-5.For the dose res... |
US Patent US10550100 (2020)
BindingDB Entry DOI: 10.7270/Q2D2211N |
More data for this Ligand-Target Pair | |
A disintegrin and metalloproteinase with thrombospondin motifs 6
(Human) | BDBM429684
(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)Show SMILES Clc1cc(Cl)cc(c1)C1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1 Show InChI InChI=1S/C20H23Cl2N3O3/c21-15-9-13(10-16(22)11-15)12-4-7-25(8-5-12)17(26)3-6-20(14-1-2-14)18(27)23-19(28)24-20/h9-12,14H,1-8H2,(H2,23,24,27,28) | UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 75 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description The basis for the assay is the cleavage of the substrate 520 MMP FRET substrate XII by human ADAMTS6.The substrate contains sequence Arg-Pro-Lys-Pro-... |
US Patent US10550100 (2020)
BindingDB Entry DOI: 10.7270/Q2D2211N |
More data for this Ligand-Target Pair | |
Disintegrin and metalloproteinase domain-containing protein 17
(Homo sapiens (Human)) | BDBM429684
(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)Show SMILES Clc1cc(Cl)cc(c1)C1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1 Show InChI InChI=1S/C20H23Cl2N3O3/c21-15-9-13(10-16(22)11-15)12-4-7-25(8-5-12)17(26)3-6-20(14-1-2-14)18(27)23-19(28)24-20/h9-12,14H,1-8H2,(H2,23,24,27,28) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | >100 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description The basis for the assay is the cleavage of the substrate 5FAM-LAQAVRSSSRK-5TAMRA (SEQ ID No 3) (Anaspec, custom 34891) by human TACE (R&D SYSTEMS INC... |
US Patent US10550100 (2020)
BindingDB Entry DOI: 10.7270/Q2D2211N |
More data for this Ligand-Target Pair | |
Collagenase 3
(Homo sapiens (Human)) | BDBM429684
(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)Show SMILES Clc1cc(Cl)cc(c1)C1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1 Show InChI InChI=1S/C20H23Cl2N3O3/c21-15-9-13(10-16(22)11-15)12-4-7-25(8-5-12)17(26)3-6-20(14-1-2-14)18(27)23-19(28)24-20/h9-12,14H,1-8H2,(H2,23,24,27,28) | PDB MMDB
NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | >100 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat# AS-27076) by human MMP13 (Chemicon, Cat#CC068).For th... |
US Patent US10550100 (2020)
BindingDB Entry DOI: 10.7270/Q2D2211N |
More data for this Ligand-Target Pair | |
A disintegrin and metalloproteinase with thrombospondin motifs 5
(Homo sapiens (Human)) | BDBM429684
(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)Show SMILES Clc1cc(Cl)cc(c1)C1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1 Show InChI InChI=1S/C20H23Cl2N3O3/c21-15-9-13(10-16(22)11-15)12-4-7-25(8-5-12)17(26)3-6-20(14-1-2-14)18(27)23-19(28)24-20/h9-12,14H,1-8H2,(H2,23,24,27,28) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 124 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.0c02008 BindingDB Entry DOI: 10.7270/Q21R6VBM |
More data for this Ligand-Target Pair | |